Chalcogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 546/278.4)
-
Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
-
Patent number: 7868178Abstract: The present invention is directed to novel cyclic amine compounds represented by the formula [I]: wherein R1 represents, but is not limited to, a hydroxyl, a halogen atom, a cyano group, a nitro group, a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 haloalkyl group, a C1-6 haloalkenyl group, a C1-6 alkylcarbonyl group, among other substituents; R2 represents a halogen atom, a nitro group, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 haloalkyl group, a five or six membered heterocyclic group having at least one hetero atom selected from an oxygen atom, a nitrogen atom, and a sulfur atom, k represents 0 or an integer of 1 to 4; R3, R31, R4, R41, R5, R51, and R7 each independently represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxycarbonyl group, or a C1-6 alkoxy group, and, both R3 and R4, may be bound together to form a saturated ring, X represents an oxygen atom, a sulfur atom, a sulfinyl group, or a sulfonyl group, a salt or an N-oxide of the chemicaType: GrantFiled: December 11, 2008Date of Patent: January 11, 2011Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa
-
Patent number: 7858621Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: GrantFiled: July 27, 2007Date of Patent: December 28, 2010Assignee: Amorepacific CorporationInventors: Sun-Young Kim, Jin Kwan Kim, Ki-Wha Lee, Byoung Young Woo, Song Seok Shin, Joo-Hyun Moh, Sung-Il Kim, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Jun Yong Ha, Hyun-Ju Koh, Young-Ho Park, Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh
-
Patent number: 7855290Abstract: A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen or the like.Type: GrantFiled: August 23, 2006Date of Patent: December 21, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Keiko Takahashi, Setsuo Funasaka, Shuji Shirotori
-
Publication number: 20100316573Abstract: A method to predict which patients will respond to a IAP inhibiting compound comprising: a) administering an IAP inhibitor compound to a patient, and b) measuring TNF-? or IL-? levels.Type: ApplicationFiled: October 17, 2007Publication date: December 16, 2010Inventors: Larry Alexander Gaither, Vadim Iourgenko, Mark Aron Labow, Dale Alan Porter, Christopher Sean Straub, Yao Yao, Leigh Zawel
-
Publication number: 20100305097Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.Type: ApplicationFiled: July 28, 2010Publication date: December 2, 2010Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
-
Publication number: 20100286146Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: April 27, 2010Publication date: November 11, 2010Applicant: Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger
-
Patent number: 7825264Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.Type: GrantFiled: December 12, 2007Date of Patent: November 2, 2010Assignee: sanofi-aventisInventors: Joachim Brendel, Heinrich Christian Englert, Stefan Peukert, Klaus Wirth, Michael Wagner, Jean-Marie Ruxer, Fabienne Pilorge
-
Patent number: 7825255Abstract: The invention relates to the compounds of formula (I), to a method for producing the same and to the use thereof as medicaments.Type: GrantFiled: February 28, 2002Date of Patent: November 2, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stásch
-
Publication number: 20100273724Abstract: This invention is directed to PEGlyated derivatives, drug conjugates and isotopic derivatives of certain ion channel modulating compounds.Type: ApplicationFiled: July 7, 2010Publication date: October 28, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M.C. Plouvier, Aregahegn S. Yifru
-
Patent number: 7820699Abstract: The invention is concerned with cyclic amines of formula (I) wherein X1 to X3, Y1 to Y3, R1?, R1? and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments and for treating diseases associated with coagulation factor Xa.Type: GrantFiled: April 13, 2006Date of Patent: October 26, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin, Beat Wirz
-
Publication number: 20100261721Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Inventors: Thomas MAIER, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
-
Publication number: 20100256198Abstract: The present invention relates to methods and compositions of metadoxine and physiologically compatible active derivatives thereof, and their use for decreasing symptoms of alcohol consumption as well as in the prevention of alcohol consumption related symptoms in subjects in need thereof.Type: ApplicationFiled: July 3, 2008Publication date: October 7, 2010Applicant: ALCOBRA LTD.Inventors: Gur Megiddo, Dalia Megiddo, Rina Yamin, Yaron Ilan, Shimon Amselem
-
Publication number: 20100247653Abstract: The present invention relates to nanoparticles containing nicotine and/or cotinine. The present invention further relates to dispersions containing these nanoparticles. The invention relates in particular to corresponding novel transdermal pharmaceuticals containing nicotine and cotinine in nanoparticulate form, and use thereof for smoking cessation.Type: ApplicationFiled: April 11, 2007Publication date: September 30, 2010Inventors: Hans Lautenschlager, Ilan Elias
-
Publication number: 20100234429Abstract: The invention relates to substituted nicotinamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRÜNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Gregor Bahrenberg, Wolfgang Schröder
-
Publication number: 20100234431Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.Type: ApplicationFiled: February 19, 2010Publication date: September 16, 2010Applicant: National Health Research InstitutesInventors: Weir-Tong Jiaang, Xin Chen
-
Publication number: 20100228035Abstract: One aspect of the present invention relates to ionic liquids comprising a pendant Bronsted-acidic group, e.g., a sulfonic acid group. Another aspect of the present invention relates to the use of an ionic liquid comprising a pendant Bronsted-acidic group to catalyze a Bronsted-acid-catalyzed chemical reaction. A third aspect of the present invention relates to ionic liquids comprising a pendant nucleophilic group, e.g., an amine. Still another aspect of the present invention relates to the use of an ionic liquid comprising a pendant nucleophilic group to catalyze a nucleophile-assisted chemical reaction. A fifth aspect of the present invention relates to the use of an ionic liquid comprising a pendant nucleophilic group to remove a gaseous impurity, e.g., carbon dioxide, from a gas, e.g., sour natural gas.Type: ApplicationFiled: February 26, 2010Publication date: September 9, 2010Applicant: University of South AlabamaInventor: James Hillard Davis, JR.
-
Publication number: 20100216815Abstract: A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 30, 2008Publication date: August 26, 2010Inventors: Joseph L. Duffy, Scott B. Hoyt, Clare London
-
Patent number: 7776891Abstract: Compounds of Formula (I) are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.Type: GrantFiled: August 12, 2005Date of Patent: August 17, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Weichao Chen, Alec D. Lebsack, Benito Munoz, Shankar Venkatraman, Bowei Wang
-
Patent number: 7767699Abstract: The invention provides a compound of formula (I): (where R1, Q, A and R2 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Pyridine-alkynyl Compound”); pharmaceutical compositions comprising an effective amount of a Pyridine-alkynyl Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, a seizure, stroke, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Pyridine-alkynyl Compound.Type: GrantFiled: December 22, 2005Date of Patent: August 3, 2010Assignee: Purdue Pharma, L.P.Inventors: Donald J. Kyle, Qun Sun, Xiaoming Zhou
-
Publication number: 20100190230Abstract: Compounds and related compositions and methods as can be used to inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.Type: ApplicationFiled: January 25, 2010Publication date: July 29, 2010Inventors: Richard B. Silverman, Fengtian Xue
-
Publication number: 20100184764Abstract: The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.Type: ApplicationFiled: March 19, 2010Publication date: July 22, 2010Applicant: ELI LILLY AND COMPANYInventors: Thomas Daniel AICHER, Mark Joseph CHICARELLI, Ronald Jay HINKLIN, Hongqi TIAN, Owen Brendan WALLACE, John Gordon ALLEN, Zhaogen CHEN, Thomas Edward MABRY, Jefferson Ray MCCOWAN, Nancy June SNYDER, Leonard Larry WINNEROSKI, JR.
-
Publication number: 20100125094Abstract: The present invention relates to new pyrrolidinyl modulating nicotinic acetylcholine receptor compounds, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 16, 2009Publication date: May 20, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr M. Shahbaz, Craig Hodulik
-
Publication number: 20100104504Abstract: The subject invention concerns materials and methods for treating and/or preventing diseases associated with accumulation of A? peptide in neural tissue. The subject invention also concerns materials and methods for treating and/or preventing stress disorders, such as post-traumatic stress disorder (PTSD). In one embodiment, a method of the invention comprises administering a therapeutically effective amount of cotinine, or a pharmaceutically acceptable salt thereof, to a person or animal in need of treatment. The methods of the invention can be used to prevent and/or treat Alzheimer's disease, Parkinson's disease, and/or Down's syndrome. The subject invention also concerns compositions that comprise cotinine, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent or adjuvant.Type: ApplicationFiled: September 24, 2009Publication date: April 29, 2010Applicants: University of South Florida, United States Department of Veterans AffairsInventor: Valentina Echeverria Moran
-
Patent number: 7687508Abstract: This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.Type: GrantFiled: July 25, 2007Date of Patent: March 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney, John Hynes, Soo S. Ko, Anurag S. Srivastava, Zili Xiao, Michael G. Yang
-
Patent number: 7674474Abstract: Pesticidal Compounds The invention relates to 1-aryl-5-disubstituted-aminopyrrole derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).Type: GrantFiled: December 22, 2006Date of Patent: March 9, 2010Assignee: Merial LimitedInventors: David Chou, Werner Knauf, Michael Maier, Michael James Malaska, Don McIntyre, Friederike Lochhaas, Scot Kevin Huber
-
Patent number: 7666868Abstract: Compounds of a certain formula (I) in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: GrantFiled: March 14, 2006Date of Patent: February 23, 2010Assignee: 4SC AGInventors: Thomas Maier, Thomas Bär, Thomas Beckers, Astrid Zimmermann, Siegfried Schneider, Volker Gekeler
-
Patent number: 7659268Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: May 18, 2007Date of Patent: February 9, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
-
Publication number: 20100016375Abstract: Compound and pharmaceutical compositions of Formula by blockade of the CB1 receptors via an inverse agonism mechanism, and are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and have increased bioavailability.Type: ApplicationFiled: October 22, 2007Publication date: January 21, 2010Inventors: John Mehnert Schaus, Perry Clark Heath
-
Publication number: 20100010222Abstract: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).Type: ApplicationFiled: August 27, 2009Publication date: January 14, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Toru MARUYAMA, Kaoru Kobayashi, Tohru Kambe, Takayuki Maruyama, Hideyuki Yoshida, Akio Nishiura, Nobutaka Abe
-
Publication number: 20090324569Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: December 31, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
-
Publication number: 20090286973Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.Type: ApplicationFiled: July 2, 2009Publication date: November 19, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah MANOHARAN, Venkitasamy KESAVAN, Kallanthottathil G. RAJEEV
-
Publication number: 20090275618Abstract: Compounds and pharmaceutical compositions of Formula (I) by blockade of the CB1 receptors via an inverse agonism mechanism which are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and have increased bioavailability.Type: ApplicationFiled: October 22, 2007Publication date: November 5, 2009Inventors: David Scott Coffey, Jingdan Hu, Stacy Jo Keding, Joseph Herman Krushinski, JR., John Mehnert Schaus, David Edward Tupper
-
Publication number: 20090270393Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: April 22, 2009Publication date: October 29, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: MASATO YOSHIDA, NOBUKI SAKAUCHI, AYUMU SATO
-
Publication number: 20090263353Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.Type: ApplicationFiled: September 8, 2006Publication date: October 22, 2009Applicant: Nycomed GmbHInventors: Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Muller, Thomas Bar, Jurgen Volz
-
Patent number: 7598250Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Type: GrantFiled: August 4, 2004Date of Patent: October 6, 2009Assignee: Schering CorporationInventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
-
Publication number: 20090239911Abstract: The present invention discloses novel compounds of Formula I: having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 24, 2007Publication date: September 24, 2009Inventors: Owen Brendan Wallace, Yanping Xu, Nancy June Snyder, Jeremy Schulenburg York, Alexei Pavlovych Krasutsky
-
Patent number: 7592358Abstract: Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.Type: GrantFiled: April 13, 2005Date of Patent: September 22, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Stenkamp, Stephan Georg Mueller, Philipp Lustenberger, Thorsten Lehmann-Lintz, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Leo Thomas, Ralf Lotz
-
Publication number: 20090221820Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: ApplicationFiled: December 12, 2008Publication date: September 3, 2009Applicant: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
-
Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
-
Publication number: 20090181929Abstract: The present invention provides a compound of formula (I): said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: ApplicationFiled: May 10, 2007Publication date: July 16, 2009Inventors: Kazuhide Konishi, Yuki Iwaki
-
Publication number: 20090172897Abstract: The disclosure relates to the dyeing of keratin materials using styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dyes. Disclosed herein is a dye composition comprising a styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dye and a dyeing process with, for example, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are novel thiol/disulfide fluorescent dyes and the uses thereof in lightening keratin materials. This composition makes it possible to obtain a lightening effect which can be resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: July 9, 2009Inventors: Nicolas DAUBRESSE, Andrew GREAVES, Franco MANFRE
-
Publication number: 20090163555Abstract: Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumours, bacterial, fungal or viral infections, or autoimmune diseases.Type: ApplicationFiled: April 20, 2007Publication date: June 25, 2009Applicant: PRODIMED, S.A.Inventors: Julio Álvarez Builla Gómez, José Luis Novella Robisco, Ma Paz Matia Martin, Sonia Serna Pereda
-
Publication number: 20090143443Abstract: The present invention is directed to novel cyclic amine compounds represented by the formula [I]: wherein R1 represents, but is not limited to, a hydroxyl, a halogen atom, a cyano group, a nitro group, a formyl group, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 haloalkyl group, a C1-6 haloalkenyl group, a C1-6 alkylcarbonyl group, among other substituents; R2 represents a halogen atom, a nitro group, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 haloalkyl group, a five or six membered heterocyclic group having at least one hetero atom selected from an oxygen atom, a nitrogen atom, and a sulfur atom, k represents 0 or an integer of 1 to 4; R3, R31, R4, R41, R5, R51, and R7 each independently represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxycarbonyl group, or a C1-6 alkoxy group, and, both R3 and R4, may be bound together to form a saturated ring, X represents an oxygen atom, a sulfur atom, a sulfinyl group, or a sulfonyl group, a salt or an N-oxide of the chemicaType: ApplicationFiled: December 11, 2008Publication date: June 4, 2009Applicant: NIPPON SODA CO., LTD.Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa
-
Publication number: 20090137806Abstract: The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.Type: ApplicationFiled: January 29, 2009Publication date: May 28, 2009Inventors: Torsten Hoffmann, Andreas Koblet, Jens-Uwe Peters, Patrick Schnider, Andrew Sleight, Heinz Stadler
-
Patent number: 7538223Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: August 4, 2006Date of Patent: May 26, 2009Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, Alex Muci, Erica Kraynack, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, Jr.
-
Publication number: 20090117074Abstract: The invention relates to compounds of formula (I) which are effective inhibitors of histone deacetylases.Type: ApplicationFiled: April 7, 2006Publication date: May 7, 2009Applicant: NYCOMED GmbHInventors: Thomas Maier, Thomas Bar, Thomas Beckers, Astrid Zimmermann, Frank Dullweber, Volker Gekeler
-
Publication number: 20090093462Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 19, 2005Publication date: April 9, 2009Inventors: Ulricn Abel, Holger Deppe, Achim Feurer, Ulrich Gradler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
-
Publication number: 20090069376Abstract: Substituted N—[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.Type: ApplicationFiled: April 17, 2006Publication date: March 12, 2009Inventors: Ping Liu, Carrie Jones, Thomas S. Reger
-
Patent number: 7479559Abstract: The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula I wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13 X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.Type: GrantFiled: March 17, 2005Date of Patent: January 20, 2009Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Stephane Caron, Christopher John Helal, Jeffrey W. Raggon, Yong Tao, Nga M. Do